This will be a Phase 1, open-label, nonrandomized, single-dose study in healthy male subjects to evaluate the Absorption, Metabolism, and Excretion of Poziotinib following a single oral dose of \[14C\]-poziotinib to healthy male subjects.
Potential subjects will be screened to assess their eligibility to enter the study within 28 days prior to the dose administration. Subjects will be admitted into the Clinical Research Unit (CRU) on Day -1. On the morning of Day 1, all subjects will receive a single oral dose of 8 mg (as the hydrochloride salt) containing approximately 100 μCi of \[14C\]-poziotinib in the fasted state. Subjects will be confined to the CRU until at least Day 8. Subjects will be discharged from the CRU on Day 8 if the following criteria are met: * ≥90% mass balance recovery in combined urine and feces, and * ≤1% of the total radioactive dose is recovered in combined excreta (urine and feces) in 2 consecutive 24-hour periods in which fecal and urine samples are obtained. If these criteria are not met by Day 8, subjects will remain in the CRU until all discharge criteria are met up to a maximum of Day 15 in order to continue 24-hour blood, urine, and feces collections, unless otherwise agreed upon by the Sponsor and Investigator.
Study Type
INTERVENTIONAL
Allocation
NA
Purpose
BASIC_SCIENCE
Masking
NONE
Enrollment
8
Single oral administration of 8 mg (as the hydrocholoride salt) of \[14C\]-poziotinib
Covance Clinical Research Unit, Inc.
Madison, Wisconsin, United States
Maximum Observed Plasma Concentration (Cmax) of [14C]-Poziotinib, Metabolites M1 and M2
Time frame: 1-15 days
Cmax of Total Radioactivity of [14C]-Poziotinib in Whole Blood and Plasma
Time frame: 1-15 days
Time to Attain Maximum Observed Plasma Concentration (Tmax) of [14C]-Poziotinib, Metabolites M1 and M2
Time frame: 1-15 days
Tmax of Total Radioactivity of [14C]-Poziotinib in Whole Blood and Plasma
Time frame: 1-15 days
Area Under the Plasma Concentration-Time Curve From Time Zero to Last Quantifiable Concentration (AUC[last]) of [14C]-Poziotinib, Metabolites M1 and M2
Time frame: 1-15 days
AUC(last) of Total Radioactivity of [14C]-Poziotinib in Whole Blood and Plasma
Time frame: 1-15 days
Area Under the Plasma Concentration-Time Curve From Time Zero to Infinity (AUCinf) of [14C]-Poziotinib, Metabolites M1 and M2
Time frame: 1-15 days
AUC(inf) of Total Radioactivity of [14C]-Poziotinib in Whole Blood and Plasma
Time frame: 1-15 days
Percentage of AUCinf Derived by Extrapolation (%AUCext) of [14C]-Poziotinib, Metabolites M1 and M2
Time frame: 1-15 days
%AUCext of Total Radioactivity of [14C]-Poziotinib in Whole Blood and Plasma
Time frame: 1-15 days
Apparent Terminal Elimination Half-Life (t1/2) of [14C]-Poziotinib, Metabolites M1 and M2
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Time frame: 1-15 days
t1/2 of Total Radioactivity of [14C]-Poziotinib in Whole Blood and Plasma
Time frame: 1-15 days
Elimination Rate Constant (λz, or kel) of [14C]-Poziotinib, Metabolites M1 and M2
Time frame: 1-15 days
λz, or kel of Total Radioactivity of [14C]-Poziotinib in Whole Blood and Plasma
Time frame: 1-15 days
Apparent Volume of Distribution (VZ/F) During Terminal Phase of [14C]-Poziotinib
Time frame: 1-15 days
Apparent Oral Clearance (CL/F) of [14C]-Poziotinib
Time frame: 1-15 days
Whole Blood : Plasma Concentration Ratios of Total Radioactivity of [14C]-Poziotinib
Time frame: 1-15 days
Total Radioactivity of Cumulative Amount Excreted in Urine (Aeu)
Time frame: 1-15 days
Total Radioactivity of Fraction of Dose Excreted in Urine (feu)
Time frame: 1-15 days
Total Radioactivity of Cumulative Amount Excreted in Feces (Aef)
Time frame: 1-15 days
Total Radioactivity of Fraction of Dose Excreted in Feces (fef)
Time frame: 1-15 days
Total Radioactivity of Cumulative Total Amount Excreted (Aetotal)
Time frame: 1-15 days
Total Radioactivity of Fraction of Dose Excreted in Urine and Feces (fetotal)
Time frame: 1-15 days
Poziotinib Metabolite Profiling and Identification in Plasma
Time frame: 1-15 days
Number of Participants with Adverse Events (AEs)
Time frame: 1-15 days
Number of Participants with Hematology, Clinical Chemistry, Urinalysis Laboratory Abnormalities
Time frame: 1-15 days
Number of Participants with 12-lead electrocardiograms (ECG) Abnormalities
Time frame: 1-15 days
Number of Participants with Vital Sign and Physical Examinations Abnormalities
Time frame: 1-15 days